In 2008,Kimball, F. Scott; Romero, F. Anthony; Ezzili, Cyrine; Garfunkle, Joie; Rayl, Thomas J.; Hochstatter, Dustin G.; Hwang, Inkyu; Boger, Dale L. published 《Optimization of α-Ketooxazole Inhibitors of Fatty Acid Amide Hydrolase》.Journal of Medicinal Chemistry published the findings.Recommanded Product: 29682-15-3 The information in the text is summarized as follows:
A series of α-ketooxazoles, e.g., I, containing conformational constraints in the flexible C2 acyl side chain of II (OL-135) and representative oxazole C5 substituents were prepared and examined as inhibitors of fatty acid amide hydrolase (FAAH). Exceptionally potent and selective FAAH inhibitors emerged from the series (e.g., 6, Ki = 200 and 260 pM for rat and rhFAAH). With simple and small C5 oxazole substituents, each series bearing a biphenylethyl, phenoxyphenethyl, or (phenoxymethyl)phenethyl C2 side chain was found to follow a well-defined linear relationship between -log Ki and Hammett σp of a magnitude (ρ = 2.7-3.0) that indicates that the substituent electronic effect dominates, confirming its fundamental importance to the series and further establishing its predictive value. Just as significantly, the nature of the C5 oxazole substituent substantially impacts the selectivity of the inhibitors whereas the effect of the C2 acyl chain was more subtle but still significant even in the small series examined Combination of these independent features, which display generalized trends across a range of inhibitor series, simultaneously improves FAAH potency and selectivity and can provide exquisitely selective and potent FAAH inhibitors. In the experiment, the researchers used Methyl 5-bromopicolinate(cas: 29682-15-3Recommanded Product: 29682-15-3)
Methyl 5-bromopicolinate(cas: 29682-15-3) belongs to pyridine. Pyridine is a relatively complex molecule and exhibits a number of different bands in IR spectra. Among others, the bands characterizing the ν8a and ν19b modes have been found to be sensitive to the coordination or protonation of the molecule. Note that the band that is diagnostic for the PyH+ ion at about 1545 cm− 1 (ν19b mode) does not overlap with any of the other bands.Recommanded Product: 29682-15-3